Screening of Chitosan Derivatives-Carbon Dots Based on Antibacterial Activity and Application in Anti-Staphylococcus aureus Biofilm

Dan Zhao,1,2 Rui Zhang,1,2 Xuemei Liu,1,2 Xiaoyun Li,1,2 Mengyu Xu,1,2 Xianju Huang,1,2 Xincai Xiao1,2 1School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan, 430074, People’s Republic of China; 2National Demonstration Center for Experimental Ethnopharmacology Education (South-Central University for Nationalities), Wuhan, 430065, People’s Republic of ChinaCorrespondence: Dan Zhao, Tel +1 806 208 4690, Email wqzhdpai@163.comIntroduction: Pathogenic bacteria, especially the ones with highly organized, systematic aggregating bacteria biofilm, would cause great harm to human health. The development of highly efficient antibacterial and antibiofilm functional fluorescent nanomaterial would be of great significance.Methods: This paper reports the preparation of a series of antibacterial functional carbon dots (CDs) with chitosan (CS) and its derivatives as raw materials through one-step route, and the impact of various experiment parameters upon the optical properties and the antibacterial abilities have been explored, including the structures of the raw materials, excipients, and solvents.Results: The CDs prepared by quaternary ammonium salt of chitosan (QCS) and ethylenediamine (EDA) exhibit multiple antibacterial effects through membrane breaking, DNA and protein destroying, and the production of singlet oxygen. The CDs showed excellent broad-spectrum inhibitory activity against a variety of bacteria (Gram-positive and negative bacteria), in particular, to the biofilm of Staphylococcus aureus with minimum inhibitory concentration at 10 μg/mL, showing great potential in killing bacteria and biofilms. The biocompatibility experiments proved that QCS-EDA-CDs are non-toxic to human normal hepatocytes and have low haemolytic effect. Furthermore, the prepared QCS-EDA-CDs have been successfully used in bacterial and biofilm imaging thanks to their excellent optical properties.Conclusion: This paper explored the preparation and application of functional CDs, which can be used as the visual probe and therapeutic agents in the treatment of infections caused by bacteria and biofilm.Graphical Abstract: Keywords: carbon dots, antibacterial activity, bacterial imaging, anti-biofilm, antibacterial mechanism